Formulations for oral administration of active agents

a technology for oral administration and active agents, applied in the field of drug delivery, can solve problems such as problematic oral administration of peptide pharmaceuticals, and achieve the effect of bioavailability of therapeutically active agents

Active Publication Date: 2018-01-25
ENTERA BIO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0048]According to some embodiments of the invention, each of the aforementioned compositions dissolves in gastric fluid in no more than 60 minutes.
[0049]According to some embodiments of the invention, absorption of the therapeutically active agent following the co-administering is characterized by a bioavailability of

Problems solved by technology

Oral administration of peptide pharmaceuticals is problematic due to degradation of pe

Method used

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  • Formulations for oral administration of active agents
  • Formulations for oral administration of active agents
  • Formulations for oral administration of active agents

Examples

Experimental program
Comparison scheme
Effect test

example 1

Effect of Antacid on Release of SNAC

[0382]Two tablet formulations were prepared, having the same amounts of SNAC, trypsin inhibitor and teriparatide (parathyroid hormone (1-34)), wherein one formulation further contained 100 mg sodium bicarbonate and the other formulation did not contain sodium bicarbonate. The tablets were in a form of a homogeneous mixture.

[0383]Each tablet formulation was subjected to a dissolution test in 100 ml of simulated gastric buffer (without pepsin), pH 2.0, at 37° C., according to USP 23 Apparatus 2 (paddle) with 50 rotations per minute. The amount of released SNAC in each sample was determined chromatographically, using an HPLC apparatus with Cosmosil™ 5 C18-MS-II (4.6 ID×250 mm) column. Mobile phase consisted of 50% acetonitrile and 50% phosphoric acid solution (0.1%). Flow rate was 1 ml / minute and injection volume was 25 μl. Amount of released SNAC was calculated as a percentage of the amount of SNAC in the formulation.

[0384]As shown in FIG. 8, sodium...

example 2

Effect of Antacid on Pharmacokinetic Profile of Orally Administered Parathyroid Hormone (PTH)

[0386]An open label comparative pharmacokinetic study was performed on ten healthy volunteers. On different visits, each volunteer received the same oral tablet containing 0.75 mg of teriparatide, a recombinant form of parathyroid hormone (1-34) (PTH(1-34)). In the first visit, the tablet was administered with 150 ml water, whereas in the second visit the tablet was administered with 150 ml of 3 mg / ml sodium bicarbonate aqueous solution.

[0387]The formulation was composed of teriparatide (0.75 mg), SNAC (sodium 8-N-(2-hydroxybenzoyl)aminocaprylate), soybean trypsin inhibitor (SBTI) and a small amount of magnesium stearate.

[0388]Tablets were administered in the morning after an 8-hour overnight fast. At each visit a standard meal was provided 3 hours after drug administration. Patients did not eat nor drink alcoholic or caffeinated beverages. There was a two week period between the two visits....

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Abstract

A pharmaceutical composition for oral administration is disclosed herein, comprising a therapeutically active agent, SNAC and at least one antacid compound. Further disclosed herein is a pharmaceutical composition unit dosage form for oral administration of a therapeutically active agent is provided herein, the unit dosage form comprising: a core comprising the therapeutically active agent and SNAC (sodium 8-N-(2-hydroxybenzoyl)aminocaprylate); and an external layer comprising at least one protective agent selected from the group consisting of an antacid compound and a protease inhibitor. Methods and uses utilizing the aforementioned pharmaceutical compositions, as well as methods and uses utilizing co-administration, by oral administration, of at least one antacid composition, and a composition comprising the therapeutically active agent and SNAC, are further disclosed herein, for use in treating a condition treatable by oral administration of the therapeutically active agent.

Description

FIELD AND BACKGROUND OF THE INVENTION[0001]The present invention, in some embodiments thereof, relates to drug delivery, and more particularly, but not exclusively, to formulations and / or systems for oral administration of therapeutically active agents such as, for example, therapeutically active polypeptides (e.g., proteins).[0002]Oral administration of peptide pharmaceuticals is problematic due to degradation of peptides and / or proteins in the digestive system and poor absorption of large molecules.[0003]U.S. Patent Application Publication No. 2007 / 0087957 describes compositions for oral administration of a protein, the compositions comprising a protein and an omega-3 fatty acid, as well as the use of such compositions for oral administration of insulin.[0004]Qi & Ping [J Microencapsulation 2004, 21:37-45] describe administration of enteric microspheres containing insulin with SNAC (sodium 8-N-(2-hydroxybenzoyl)aminocaprylate). The enteric microspheres are for protecting the insul...

Claims

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Application Information

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IPC IPC(8): A61K31/166A61K31/05A61K9/28A61K38/22A61K9/00A61K9/20A61K31/19A61K38/55
CPCA61K31/166A61K31/19A61K31/05A61K38/55A61K38/22A61K9/0053A61K9/2009A61K9/2013A61K9/2086A61K9/2886A61K2300/00A61K38/29A61P19/10A61K31/195A61K45/06A61K9/28A61K47/12A61P5/18A61K9/2054A61K9/20A61K31/20
Inventor BURSHTEIN, GREGORYROTHNER, ARIELSCHWARTZ, PHILIP M.GALITZER, HILLEL
Owner ENTERA BIO LTD
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